Veterinary aqueous injectable suspensions containing florfenicol

Abstract

The present invention relates to pharmaceutical compositions in the form of aqueous injectable suspensions for veterinary use, comprising sterile and micronized florfenicol or a substantially water-insoluble complex in a concentration up to 500 mg / ml. , co-crystalline or salt form of florfenicol. The suspension can achieve parenteral antibacterial treatment of animals with excellent overall and local tolerability through a limited number of injections. The suspension had limited settling on standing and after transport, was easily resuspended, and had good injectability.

Description

technical field [0001] The present invention relates to a pharmaceutical composition for veterinary use containing a high concentration of florfenicol as a pharmaceutically active ingredient, more particularly said composition is an aqueous injectable suspension. Background technique [0002] Florfenicol [D-(threo)-1-p-methylsulfonylphenyl-2-dichloroacetamido-3-fluoro-1-propanol] is an antibacterial agent known to be commonly used for veterinary purposes. Florfenicol is a broad-spectrum antibiotic active to a variety of pathogenic veterinary bacteria (NEU et al., Antimicrob. 19, 2, 294-297). [0003] Injectable formulations containing florfenicol have been described in several patents. [0004] European Patent 0 014 437 B1 discloses not only the synthesis of Florfenicol but also examples of different formulations, including oral suspensions, injectable solutions in water / dimethylacetamide mixtures and instant reconstituted bacteria powder. [0005] European Patent 0 546 ...

AI Technical Summary

Problems solved by technology

[0006] Although the formulation reportedly exhibited acceptable tissue tolerance at the injection site, it was considered painful by licensed veterinarians to inject the formulation

[0007] Although the injectable formulation described in European patent 0 546 018 B1 may improve the previous injectable solution (such as the preparation dissolved in pure N-methyl-2-pyrrolidone), if combined with other physiologically acceptable Said formulations are also very irritating and irritating compared to aqueous solutions and suspensions (containing lower concentrations of physiologically acceptable solvents, having a physiologically acceptable pH, and having significantly lower osmotic pressure at the injection site). painful